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Assay Detail

CHEMBL664532

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Binding
Inhibitory activity against dipeptidylpeptidase IV.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Dipeptidyl peptidase 4 (CHEMBL284)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.
Parmee ER, He J, Mastracchio A, Edmondson SD, Colwell L, Eiermann G, Feeney WP, Habulihaz B, He H, Kilburn R, Leiting B, Lyons K, Marsilio F, Patel RA, Petrov A, Di Salvo J, Wu JK, Thornberry NA, Weber AE.
Bioorg Med Chem Lett (2004) 14 : 43 -46
PubMed 14684294 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 7.42 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL497992 1 8.59
CHEMBL3084937 1 8.12
CHEMBL3084956 1 8.05
CHEMBL3084953 1 8.00
CHEMBL3084949 1 7.82
CHEMBL3084952 1 7.77
CHEMBL3084954 1 7.77
CHEMBL3084942 1 7.75
CHEMBL3084951 1 7.70
CHEMBL3084948 1 7.68
CHEMBL25211 1 7.66
CHEMBL77538 1 7.66
CHEMBL3084935 1 7.64
CHEMBL3084943 1 7.62
CHEMBL3084936 1 7.62
CHEMBL23176 1 7.60
CHEMBL3084938 1 7.58
CHEMBL3084950 1 7.54
CHEMBL3084947 1 7.48
CHEMBL1682974 1 7.48
CHEMBL142703 VILDAGLIPTIN 4.0 1 7.47
CHEMBL3084939 1 7.46
CHEMBL3084946 1 7.42
CHEMBL3084944 1 7.34
CHEMBL22359 1 7.28
CHEMBL3084955 1 7.26
CHEMBL3084940 1 7.19
CHEMBL25437 1 7.06
CHEMBL23979 1 7.05
CHEMBL22679 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL497992 IC50 = 2.6 nM 8.59
CHEMBL3084937 IC50 = 7.5 nM 8.12
CHEMBL3084956 IC50 = 9.0 nM 8.05
CHEMBL3084953 IC50 = 10.0 nM 8.00
CHEMBL3084949 IC50 = 15.0 nM 7.82
CHEMBL3084952 IC50 = 17.0 nM 7.77
CHEMBL3084954 IC50 = 17.0 nM 7.77
CHEMBL3084942 IC50 = 18.0 nM 7.75
CHEMBL3084951 IC50 = 20.0 nM 7.70
CHEMBL3084948 IC50 = 21.0 nM 7.68
CHEMBL25211 IC50 = 22.0 nM 7.66
CHEMBL77538 IC50 = 22.0 nM 7.66
CHEMBL3084935 IC50 = 23.0 nM 7.64
CHEMBL3084943 IC50 = 24.0 nM 7.62
CHEMBL3084936 IC50 = 24.0 nM 7.62
CHEMBL23176 IC50 = 25.0 nM 7.60
CHEMBL3084938 IC50 = 26.0 nM 7.58
CHEMBL3084950 IC50 = 29.0 nM 7.54
CHEMBL1682974 IC50 = 33.0 nM 7.48
CHEMBL3084947 IC50 = 33.0 nM 7.48
CHEMBL142703 VILDAGLIPTIN IC50 = 34.0 nM 7.47
CHEMBL3084939 IC50 = 35.0 nM 7.46
CHEMBL3084946 IC50 = 38.0 nM 7.42
CHEMBL3084944 IC50 = 46.0 nM 7.34
CHEMBL22359 IC50 = 53.0 nM 7.28
CHEMBL3084955 IC50 = 55.0 nM 7.26
CHEMBL3084940 IC50 = 64.0 nM 7.19
CHEMBL25437 IC50 = 88.0 nM 7.06
CHEMBL23979 IC50 = 89.0 nM 7.05
CHEMBL22679 IC50 = 94.0 nM 7.03
CHEMBL3084941 IC50 = 98.0 nM 7.01
CHEMBL278558 IC50 = 190.0 nM 6.72
CHEMBL278393 IC50 = 320.0 nM 6.50
CHEMBL98408 IC50 = 420.0 nM 6.38
CHEMBL3084945 IC50 = 2700.0 nM 5.57